Classifications

• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
  • C07H3/00—Compounds containing only hydrogen atoms and saccharide radicals having only carbon, hydrogen, and oxygen atoms
  • C07H3/02—Monosaccharides
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
  • A61K31/7004—Monosaccharides having only carbon, hydrogen and oxygen atoms
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
  • A23L27/00—Spices; Flavouring agents or condiments; Artificial sweetening agents; Table salts; Dietetic salt substitutes; Preparation or treatment thereof
  • A23L27/30—Artificial sweetening agents
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
  • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
  • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
  • A23L33/13—Nucleic acids or derivatives thereof
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
  • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
  • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
  • A23L33/15—Vitamins
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
  • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
  • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
  • A23L33/17—Amino acids, peptides or proteins
  • A23L33/175—Amino acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
  • A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
  • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
  • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P3/00—Drugs for disorders of the metabolism
  • A61P3/02—Nutrients, e.g. vitamins, minerals
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P9/00—Drugs for disorders of the cardiovascular system
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
  • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs

Definitions

• the present invention relates to a health food/dietary supplement comprising as its characterising ingredients an alkanoyl L-carnitine selected from the group consisting of isovaleryl L-carnitine and propionyl L-carnitine or their pharmacologically acceptable salts or mixtures of the same and a monosaccharide pentose, particularly ribose or its phosphorylated analogues.
• an alkanoyl L-carnitine selected from the group consisting of isovaleryl L-carnitine and propionyl L-carnitine or their pharmacologically acceptable salts or mixtures of the same and a monosaccharide pentose, particularly ribose or its phosphorylated analogues.
• composition is extremely effective in exerting a potent stimulation of muscular energy metabolism, and can thus be profitably used in the prevention of myocardial insufficiency and in post-infarct conditions, as well as in the course of prolonged muscular effort during physical and sporting exercises, owing to the unexpected synergistic effect exerted by its components.
• Isovaleryl L-carnitine a natural component of the pool of carnitines, presents specific activity at lysosomal level and on the cytosolic movements of calcium. It is therefore capable of intervening in proteolytic processes such as occur during intense, prolonged effort and of protecting a number of organs, such as the liver, against the action of toxic substances.
• Propionyl L-carnitine exerts an intense antioxidant effect and is particularly effective in enhancing the peripheral circulation and cardiac functional capacity.
• propionyl L-carnitine transferase possesses a greater affinity for propionyl L-carnitine than for L-carnitine, and consequently propionyl L-carnitine possesses a higher degree of specificity for cardiac and skeletal muscle.
• propionyl L-carnitine transferase transporting the propionyl group, increases the uptake of this component by the muscle cells, which may be of particular importance for energy purposes, in that the propionate can be used by the mitochondria as an anapleurotic substrate and provide energy in the absence of oxygen.
• Ribose is a monosaccharide pentose which is important in the body for the synthesis of nucleotides and other metabolic products. It is formed by conversion of glucose via the pentose phosphates.
• ribokinase ribose is phosphorylated to ribose-5-phosphate which, through the production of 5-phosphoribosyl-1-pyrophosphate (PRPP), can be used for the synthesis of nucleotides necessary for the production of ATP.
• PRPP in addition to intervening in the production of ATP, is also important for the synthesis of nucleotides such as adenine and hypoxanthine and of ribonucleotides and deoxyribo-nucleotides.
• composition comprising a combination of the following as its characterising components:
• an alkanoyl L-carnitine selected from the group comprising isovaleryl L-carnitine, propionyl L-carnitine or their pharmacologically acceptable salts or mixtures of the same;
• ribose or a phosphorylate derivative thereof constitutes an effective health food/dietary supplement for the prevention of states of myocardial or skeletal muscle dysfuntion related to conditions of anoxia or insufficient energy supply as occurring in coronary or post-bifarct disorders or during prolonged physical activity and muscle fatigue, owing to the potent and unexpected synergistic effect exerted by its components.
• the dietary supplement according to the present invention may additionally contain
• a “carnitine” selected from the group comprising L-carnitine, acetyl L-carnitine, butyryl L-carnitine and valeryl L-carnitine, or their pharmacologically acceptable salts or mixtures of the same.
• weight-to-weight ratios of the above-mentioned components (a):(b):(c) range from 1:1:1 to 1:10:2.
• this unexpected synergistic effect on the increase in energy capabilities at both cardiac and muscular level exerted by the combination according to the present invention enables it to be used in the prevention of both myocardial insufficiency and of muscle fatigue such as occur in cases of myocardial ischaemia or in the course of intense muscular effort due to prolonged physical exercise or sporting activity.
• the anoxic state was obtained by introducing 100% N 2 instead of O 2 into the bath.
• the method described by Strehler was adopted (Strehler B. L. Methods in Enzymology 111 N.Y. Acad. Press., 879, 1957).
• Coronary occlusion and the resulting myocardial anoxia lead after 5-8 minutes, to the onset of arrhythmias.
• ventricular ectopic contractions were counted for a period of 30 minutes after ligation both in control rats and in rats that had received slow injections into the left ventricle, 15 minutes before ligation, of a solution containing isovaleryl L-carnitine alone (100 mg/kg), propionyl L-carnitine alone (100 mg/kg), or carnitine combination alone consisting of propionyl L-carnitine (25 mg/kg), acetyl L-carnitine (25 mg/kg) and isovaleryl L-carnitine (25 mg/kg) or ribose alone (100 mg/kg), or a combination of ribose plus isovaleryl L-carnitine or propionyl L-carnitine or a combination of ribose plus carnitine combination at the doses described above.
• compositions according to the present invention are given hereinbelow: Lozenges, capsules, tablets 1) Propionyl L-carnitine 500 mg Ribose 500 mg 2) Isovaleryl L-carnitine 500 mg Ribose 500 mg 3) Propionyl L-carnitine 125 mg Acetyl L-carnitine 125 mg L-carnitine 125 mg Isovaleryl L-carnitine 125 mg Ribose 500 mg Granulates or vials 4) Propionyl L-carnitine 1 g Ribose 1 g 5) Isovaleryl L-carnitine 1 g Ribose 1 g 6) Propionyl L-carnitine 1 g Ribose 2.5 g 7) Propionyl L-carnitine 250 mg Acetyl L-carnitine 250 mg Isovaleryl L-carnitine 250 mg L-carnitine 250 mg Ribose 2.5 g 8) Propionyl L-carnitine 250 mg Ace
• a pharmacologically acceptable salt of the various carnitines mentioned in the present invention is, in addition to the respective inner salts, any salt of these with an acid which does not give rise to unwanted toxic or side effects.
• acids are well known to pharmacologists and to experts in pharmaceutical technology.
• Non-limiting examples of such salts are the following: chloride; bromide; iodide; aspartate, acid aspartate; citrate, acid citrate; tartrate; phosphate, acid phosphate; fumarate, acid fumarate; glycerophosphate; glucose phosphate; lactate; maleate, acid maleate; mucate; orotate; oxalate, acid oxalate; sulphate, acid sulphate; trichloroacetate; trifluoroacetate and methane sulphonate.
• isovaleryl L-carnitine acid fumarate (U.S. Pat. No. 5,227,58) is particularly preferred.
• the supplement of the invention may further comprise vitamins, coenzymes, mineral substances, aminoacids and antioxidants.
• the supplement may be manufactured in the form of tablets, lozenges, capsules, pills, granulates, syrups, vials or drops.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Engineering & Computer Science (AREA)
• General Health & Medical Sciences (AREA)
• Nutrition Science (AREA)
• Food Science & Technology (AREA)
• Organic Chemistry (AREA)
• Polymers & Plastics (AREA)
• Medicinal Chemistry (AREA)
• Veterinary Medicine (AREA)
• Pharmacology & Pharmacy (AREA)
• Animal Behavior & Ethology (AREA)
• Public Health (AREA)
• Mycology (AREA)
• Molecular Biology (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Biochemistry (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Proteomics, Peptides & Aminoacids (AREA)
• General Chemical & Material Sciences (AREA)
• Epidemiology (AREA)
• Biotechnology (AREA)
• Genetics & Genomics (AREA)
• Obesity (AREA)
• Physical Education & Sports Medicine (AREA)
• Heart & Thoracic Surgery (AREA)
• Cardiology (AREA)
• Hematology (AREA)
• Diabetes (AREA)
• Neurology (AREA)
• Orthopedic Medicine & Surgery (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Coloring Foods And Improving Nutritive Qualities (AREA)

Priority Applications (3)

Applications Claiming Priority (2)

Related Child Applications (2)

Publications (1)

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• 2000
  • 2000-06-14 IT IT2000RM000323A patent/IT1317043B1/it active
• 2001
  • 2001-01-06 US US10/048,590 patent/US20030108537A1/en not_active Abandoned
  • 2001-04-24 SK SK1729-2002A patent/SK287308B6/sk not_active IP Right Cessation
  • 2001-06-01 DE DE60103055T patent/DE60103055T2/de not_active Expired - Lifetime
  • 2001-06-01 EP EP01941001A patent/EP1292312B1/de not_active Expired - Lifetime
  • 2001-06-01 TR TR2004/01096T patent/TR200401096T4/xx unknown
  • 2001-06-01 IL IL14803801A patent/IL148038A0/xx unknown
  • 2001-06-01 CA CA002381339A patent/CA2381339C/en not_active Expired - Fee Related
  • 2001-06-01 HU HU0202496A patent/HU228642B1/hu not_active IP Right Cessation
  • 2001-06-01 PL PL352578A patent/PL199641B1/pl unknown
  • 2001-06-01 ES ES01941001T patent/ES2219531T3/es not_active Expired - Lifetime
  • 2001-06-01 MX MXPA02001550A patent/MXPA02001550A/es active IP Right Grant
  • 2001-06-01 WO PCT/IT2001/000283 patent/WO2001095915A1/en not_active Ceased
  • 2001-06-01 DK DK01941001T patent/DK1292312T3/da active
  • 2001-06-01 SK SK210-2002A patent/SK2102002A3/sk unknown
  • 2001-06-01 PT PT01941001T patent/PT1292312E/pt unknown
  • 2001-06-01 CZ CZ2002366A patent/CZ2002366A3/cs unknown
  • 2001-06-01 AT AT01941001T patent/ATE265216T1/de active
  • 2001-06-01 AU AU74487/01A patent/AU782367B2/en not_active Ceased
• 2002
  • 2002-02-13 NO NO20020731A patent/NO20020731L/no not_active Application Discontinuation
• 2006
  • 2006-11-27 US US11/604,390 patent/US20070116743A1/en not_active Abandoned
• 2010
  • 2010-04-02 US US12/753,368 patent/US8518455B2/en not_active Expired - Fee Related
• 2013
  • 2013-07-26 US US13/952,083 patent/US8747906B2/en not_active Expired - Fee Related

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